DK2855452T3 - Substituterede pyrrolidiner som faktor xia-hæmmere til behandling af tromboemboliske sygdomme - Google Patents

Substituterede pyrrolidiner som faktor xia-hæmmere til behandling af tromboemboliske sygdomme Download PDF

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DK2855452T3
DK2855452T3 DK13727822.2T DK13727822T DK2855452T3 DK 2855452 T3 DK2855452 T3 DK 2855452T3 DK 13727822 T DK13727822 T DK 13727822T DK 2855452 T3 DK2855452 T3 DK 2855452T3
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compound
formula
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alkyl
thrombosis
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Steve Courtney
Chris Yarnold
Osamu Ichihara
Stuart Flanagan
Akira Imagawa
Takashi Kondo
Taihei Nishiyama
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Ono Pharmaceutical Co
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Claims (7)

  1. SUBSTITUTEREDE PYRROLIDINER SOM FAKTOR XIA-HÆMMERE TIL BEHANDLING AF TROMBOEMBOLISKE SYGDOMME 1. 4-[({(2S,4S)-l-(4-carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)-l-piperazinyl]-2-pyrrolidinyl} carbonyl)amino]benzoesyre eller farmaceutisk acceptabelt salt deraf.
  2. 2. Farmaceutisk sammensætning, der omfatter 4-[({(2S,4S)-l-(4-carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)-l-piperazinyl]-2-pyrrolidinyl}carbonyl)amino]benzoesyre eller et farmaceutisk acceptabelt salt deraf.
  3. 3. Farmaceutisk sammensætning ifølge krav 2, til anvendelse som en faktor Xla-hæmmer.
  4. 4. Farmaceutisk sammensætning til anvendelse ifølge krav 3 i behandlingen eller forebyggelsen af en tromboembolisk sygdom.
  5. 5. 4-[({(2S,4S)-l-(4-carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)-l-piperazinyl]-2-pyrrolidinyl} carbonyl)amino]benzoesyre eller farmaceutisk acceptabelt salt deraf til anvendelse i behandling eller forebyggelse af en tromboembolisk sygdom.
  6. 6. 4-[({(2S,4S)-l-(4-carbamimidoylbenzoyl)-4-[4-(melhylsulfonyl)-l-piperazinyl]-2-pyrrolidinyl} carbonyl)amino]benzoesyre eller farmaceutisk acceptabelt salt deraf til anvendelse i behandling eller forebyggelse af en tromboembolisk sygdom, hvor den tromboemboliske sygdom er udvalgt fra gruppen bestående af arterielle kardiovaskulære tromboemboliske forstyrrelser, venøse kardiovaskulære tromboemboliske forstyrrelser, arterielle cerebrovaskulære tromboemboliske forstyrrelser, venøse cerebrovaskulære tromboemboliske forstyrrelser og tromboemboliske forstyrrelser i hjertekamrene eller i det perifere kredsløb.
  7. 7. 4-[({(2S,4S)-l-(4-carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)-l-piperazinyl]-2-pyrrolidinyl} carbonyl)amino]benzoesyre eller farmaceutisk acceptabelt salt deraf til anvendelse i behandling eller forebyggelse af en tromboembolisk sygdom, hvor den tromboemboliske sygdom er udvalgt fra dissemineret intravaskulær koagulopati (DIC), akut respirationsinsu fTicicnssyndrom, akut lungelæsion, sepsis, angina, ustabil angina, et akut koronart syndom, koronar arteriesygdom, myokardieinfarkt, atrieflimren, iskæmisk pludselig død, transient iskæmisk attack, apopleksi, akut apopleksi, lakunært infarkt, atherosklerotisk trombotisk cerebralinfarkt, atherotrombose, atherosklerose, perifer okklusiv arteriesygdom, venetrombose, dyb venetrombose, thrombophlebitis, arteriel embolisme, koronar arterietrombose, cerebral trombose, cerebral arterietrombose, cerebral embolisme, kardiogen embolisme, nyreembolisme, portåretrombose, lungeembolisme, lungeinfarkt, leverembolisme, mesenterialarterie- og/eller veneembolisme, okklusion af nethindevene og/eller -arterie, systemisk embolisme, antiphospholipid-antistofsyndrom, trombose som følge af koronararterie-bypass-graft-kirurgi og trombose som følge af medicinske implantater, anordninger eller procedurer, hvor blod eksponeres for en kunstig overflade, der fremmer trombose.
DK13727822.2T 2012-05-24 2013-05-23 Substituterede pyrrolidiner som faktor xia-hæmmere til behandling af tromboemboliske sygdomme DK2855452T3 (da)

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GBGB1209138.5A GB201209138D0 (en) 2012-05-24 2012-05-24 Compounds
PCT/EP2013/060650 WO2013174937A1 (en) 2012-05-24 2013-05-23 Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases

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US (5) US9394250B2 (da)
EP (2) EP3056493B1 (da)
JP (2) JP6142919B2 (da)
KR (1) KR102090780B1 (da)
CN (1) CN104379576B (da)
AU (1) AU2013265256B2 (da)
BR (1) BR112014027236A2 (da)
CA (1) CA2874106C (da)
DK (1) DK2855452T3 (da)
ES (2) ES2637655T3 (da)
GB (1) GB201209138D0 (da)
HK (1) HK1207854A1 (da)
HU (1) HUE034856T2 (da)
IL (1) IL235767A (da)
MX (1) MX363043B (da)
NZ (1) NZ702070A (da)
PH (1) PH12014502573B1 (da)
PL (1) PL2855452T3 (da)
PT (1) PT2855452T (da)
RU (1) RU2636050C2 (da)
SG (1) SG11201408271VA (da)
TW (1) TWI573786B (da)
WO (1) WO2013174937A1 (da)
ZA (1) ZA201408593B (da)

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